Berotek N - Instructions For The Use Of Aerosol, Price, Analogues, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Berotek N

Latin name: Berotec N

ATX code: R03AC04

Active ingredient: fenoterol (Fenoterol)

Manufacturer: Boehringer Ingelheim Pharma (Germany)

Description and photo updated: 2018-29-11

Prices in pharmacies: from 374 rubles.

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Berotek N is a selective beta ₂ -adrenomimetic, bronchodilator.

Release form and composition

Dosage form - metered-dose inhalation aerosol: clear colorless or light yellow or light brown liquid, free from suspended particles [10 ml (200 doses) each in metal aerosol cans equipped with a metering valve and mouthpiece; in a cardboard box 1 can and instructions for use Beroteka N].

Composition of 1 inhalation dose of aerosol:

• active substance: fenoterol hydrobromide - 100 mcg;
• auxiliary components: purified water, tetrafluoroethane (HFA 134a, propellant), absolute ethanol, anhydrous citric acid.

Pharmacological properties

Pharmacodynamics

The active substance of Beroteka N - fenoterol hydrobromide, is a selective beta ₂ -adrenomimetic, bronchodilator. The drug prevents and relieves attacks of bronchospasm in bronchial asthma and other diseases accompanied by airway obstruction (chronic obstructive bronchitis, including pulmonary emphysema).

Fenoterol, used in the therapeutic dose range, is a selective stimulant of β ₂ -adrenergic receptors. When using the drug in higher doses, β ₁ -adrenoreceptors are stimulated.

Due to binding to β ₂ -adrenergic receptors, adenylate cyclase is activated through the stimulatory G _s -protein, subsequently - the formation of cyclic adenosine monophosphate (cAMP) increases, which activates protein kinase A. Protein kinase A prevents the connection of myosin with actin, as a result of which smooth muscles relax.

Fenoterol relaxes the smooth muscles of the bronchi and blood vessels, and also protects against bronchoconstrictor stimuli such as allergens (early response), cold air, exercise, histamine and methacholine.

In addition, fenoterol inhibits the release of pro-inflammatory and bronchoconstrictor mediators from mast cells. After the use of fenoterol at a dose of 600 μg, an increase in mucociliary clearance was noted.

Having a stimulating effect on β ₁ -adrenergic receptors, fenoterol (especially in higher doses than therapeutic ones) can have an effect on the myocardium, causing an increase and an increase in heart rate.

The drug quickly relieves bronchospasm of various origins. The bronchodilatory effect develops within a few minutes after inhalation and lasts for 3-5 hours.

Pharmacokinetics

Depending on the inhalation system used and the technique of inhalation of the lower respiratory tract, it reaches about 10-30% of fenoterol hydrobromide, the rest of the drug settles in the mouth and upper respiratory tract, after which it is swallowed.

After inhalation of Beroteka N, the absolute bioavailability of fenoterol is 18.7%.

The absorption of the drug from the lungs occurs in two phases: 30% of the dose is absorbed quickly with a half-life (T _½) of 11 minutes, 70% - slowly with T _½ 120 minutes.

The maximum plasma concentration (C _max) of fenoterol after inhalation at a dose of 200 μg is 66.9 pg / ml and is reached within 15 minutes.

With oral administration of fenoterol hydrobromide, approximately 60% of the dose is absorbed. The absorbed amount of the substance undergoes an extensive first phase of metabolism in the liver. Thus, oral bioavailability is about 1.5%, and its contribution to the plasma concentration of the drug after inhalation is small.

Plasma proteins bind 40–55%. After intravenous (iv) administration of the drug, the distribution of fenoterol in plasma is adequately described by a 3-component pharmacokinetic model with T _½ 0.42 min, 14.3 min and 3.2 h. After IV administration, the volume of distribution (V _d) of fenoterol at equilibrium concentration is 1.9–2.7 l / kg.

Fenoterol can cross the placental barrier and be excreted in breast milk.

The drug is extensively metabolized in the liver by conjugation to glucuronides and sulfates. Part of fenoterol that has entered the gastrointestinal tract is metabolized mainly by sulfation, while the onset of metabolic activation of the parent substance occurs already in the intestinal wall.

Fenoterol is excreted in the form of inactive sulfate conjugates in urine and bile. The main part of the drug dose (approximately 85%) undergoes biotransformation. About 15% of the average total clearance of the systemically available dose is excreted in the urine. The volume of renal clearance is indicative of tubular drug secretion in addition to glomerular filtration.

After inhalation, 2% of the dose is excreted unchanged through the kidneys within 24 hours.

Indications for use

• diseases accompanied by reversible airway obstruction, including chronic obstructive pulmonary disease and chronic bronchitis;
• attacks of bronchial asthma;
• prevention of bronchial asthma attacks during physical exertion.

Contraindications

Absolute:

• hypertrophic obstructive cardiomyopathy;
• tachyarrhythmia;
• children under 4 years of age;
• hypersensitivity to any component of the drug.

Relative (aerosol Berotek N, especially in high doses, can be used only after assessing the balance of benefits and risks):

• insufficiently controlled diabetes mellitus;
• hypokalemia;
• hyperthyroidism;
• pheochromocytoma;
• severe organic diseases of the heart and blood vessels: severe lesions of peripheral and cerebral arteries, coronary artery disease, ischemic heart disease, heart defects (including aortic stenosis), chronic heart failure;
• recent myocardial infarction (in the previous 3 months);
• pregnancy and lactation;
• children age 4-6 years;
• simultaneous use of monoamine oxidase inhibitors (MAO), tricyclic antidepressants.

Berotek N, instructions for use: method and dosage

Aerosol Berotek N is used by inhalation. 1 dose = 1 injection.

Recommended dosage regimens of Beroteka N for adults and children from 6 years of age:

• bronchial asthma attacks and diseases with reversible airway obstruction: 1 dose in case of an attack. After 5 minutes, inhalation can be repeated if breathing has not been relieved. If after 2 inhalations there is no effect, you should immediately consult a doctor. During the day, you can use no more than 8 inhalation doses;
• prevention of attacks of bronchial asthma of physical exertion: 1-2 doses before physical activity, but not more than 8 doses per day.

Dosing regimen of Beroteka N for children 4-6 years old:

• bronchial asthma attacks and diseases with reversible airway obstruction: 1 dose in case of an attack. If there is no effect, you should immediately consult a doctor;
• prevention of bronchial asthma attacks of physical exertion: 1 dose before physical activity, but no more than 4 doses per day.

Achieving the maximum effect is possible only with the correct use of the inhaler. To prepare a new inhaler for use, remove the protective cap, turn the balloon upside down and double-click on its bottom (make two injections into the air). A single injection into the air must be performed if the inhaler has not been used for more than 3 days.

The following rules should be observed with every use of Berotek N:

1. Remove the protective cap.
2. Exhale fully.
3. Holding the can upside down, tightly wrap your lips around the mouthpiece.
4. Inhale as deeply as possible and simultaneously press firmly on the bottom of the balloon to release one inhalation dose. Hold your breath for a few seconds, remove the mouthpiece and exhale slowly.
5. When prescribing several doses, repeat the steps described in points 2-4.
6. Put on the protective cap.

The can is not transparent, so it is impossible to visually determine whether it is empty. Each bottle is designed for 200 doses, but after use it may contain some more of the drug. It cannot be used, since in this case there is a risk that the patient will not be able to receive the therapeutic dose he needs.

The amount of the drug remaining in the bottle can be roughly determined as follows: remove the protective cap, immerse the bottle in a container with water and look at its position. If the cylinder floats on the surface of the water, leaning to one side, it is empty; floats upside down and slightly bent to the side - contains ¼ part of the aerosol; floats upside down strictly vertically - contains ½; drowned - contains ¾.

The inhaler should be cleaned at least once a week. The mouthpiece must be clean so that the aerosol does not accumulate and block the spray.

Inhaler cleaning rules:

1. Remove the cap and remove the cartridge from the inhaler.
2. Rinse the inhaler body with warm water.
3. Shake the inhaler to remove any remaining water and let it air dry. Do not use heating devices!
4. Insert the bottle and put on the protective cap.

The plastic mouthpiece serves as a dispenser for the drug and is specially designed for the Berotek N. aerosol. It cannot be used with other aerosols; it is also forbidden to use other adapters for dosing Berotek N.

The aerosol in the can is under pressure. The cylinder must not be heated above 50 ° C and must not be opened.

Side effects

• from the respiratory system: often (from ≥ 1/100 to <1/10) - cough; infrequently (from ≥ 1/1000 to <1/100) - paradoxical bronchospasm; the frequency is unknown (the available data are insufficient to determine the frequency of development of the effects) - irritation of the larynx and pharynx;
• on the part of the cardiovascular system: infrequently - arrhythmia; the frequency is unknown - a decrease in diastolic blood pressure (BP), an increase in systolic blood pressure, palpitations, tachycardia, myocardial ischemia;
• from the digestive system: infrequently - nausea, vomiting;
• on the part of the musculoskeletal system: frequency unknown - muscle weakness, muscle spasm, myalgia;
• on the part of the psyche and nervous system: often - tremor; infrequently - excitement; frequency unknown - dizziness, headache, nervousness;
• from the side of metabolism: infrequently - hypokalemia (including severe);
• from the immune system: the frequency is unknown - urticaria, hypersensitivity;
• from the skin and subcutaneous tissues: infrequently - itching; frequency unknown - skin reactions (including rash), hyperhidrosis.

Overdose

The main symptoms of an overdose are due to excessive beta-adrenergic stimulation: a decrease or increase in blood pressure, an increase in pulse pressure, palpitations, arrhythmias, tachycardia, angina pectoris, tremors, facial flushing. Hypokalemia and metabolic acidosis are also possible.

In case of an overdose, Berotek N is canceled. The patient is prescribed sedatives, in severe cases, intensive symptomatic therapy is carried out. It is necessary to control the balance of electrolytes and acid-base balance.

As specific antidotes, it is possible to use beta-blockers (preferably selective beta ₁ -blockers). However, caution is required in the selection of the dose of these drugs, since bronchial obstruction may increase.

special instructions

The use of Beroteka N for relief of bronchial asthma attacks (for symptomatic therapy) is more preferable than regular use of the drug.

Patients should be evaluated to determine the need for or intensifying anti-inflammatory treatment (eg, inhaled glucocorticosteroids) to control airway inflammation and prevent delayed lung injury.

With increased bronchial obstruction, it is prohibited to increase the frequency of inhalation of Berotek N and its use in doses exceeding those prescribed by the doctor. This can be dangerous because the need for regular use of β ₂ -adrenoceptor agonists may be a sign of worsening disease control. In this case, a revision of the treatment plan is required, especially the adequacy of the anti-inflammatory therapy being carried out, in order to avoid the development of a potentially life-threatening deterioration in disease control.

Like any inhalation agent, Berotek N can cause a potentially life-threatening paradoxical bronchospasm. In this case, you must immediately cancel the drug and prescribe an alternative therapy.

Patients should immediately consult a doctor if they experience acute, rapidly developing shortness of breath.

Sympathomimetics, including Berotek N, can cause cardiovascular effects. There are rare reports of the development of myocardial ischemia. Patients with concomitant severe heart disease (eg, arrhythmia, severe heart failure, or coronary artery disease) should be warned to seek urgent medical attention if chest pain or worsening cardiovascular disease occurs.

Particular attention should be paid to symptoms such as chest pain and shortness of breath, as they can be both cardiac and respiratory in nature.

With beta ₂ -agonist therapy, potentially serious hypokalemia may develop. Care must be taken in patients with severe bronchial asthma, since their hypokalemia can be exacerbated by the action of concomitantly used glucocorticosteroids, diuretics, xanthine derivatives. In addition, hypoxia associated with hypokalemia can increase its effect on heart rate. In patients receiving digoxin, due to hypokalemia, an increased predisposition to arrhythmias is possible. In such cases, monitoring of serum potassium levels is required.

During the period of application of Berotek N in studies on drug abuse for non-medical indications, it is possible to obtain positive test results for the presence of fenoterol, which is important, for example, for athletes (doping control).

It is necessary to take into account a small amount of ethanol in the Berotek N aerosol: in 1 dose - 15,597 mg.

The simultaneous use of other sympathomimetic bronchodilators is allowed only as directed by a physician and under his strict supervision.

Berotec N can be used in combination with anticholinergic bronchodilators.

Influence on the ability to drive vehicles and complex mechanisms

Special studies on the effect of Berotek N on human psychophysical functions have not been carried out. However, rare cases of dizziness have been reported in clinical studies. In this regard, it is recommended to observe safety precautions while driving and performing potentially dangerous types of work.

Application during pregnancy and lactation

In preclinical and clinical studies, there was no negative effect of fenoterol on the course of pregnancy and fetal development. However, during pregnancy (especially in the first trimester), Berotek N should be used only as directed by a physician who will assess the degree of correlation between the expected benefits and possible risks. It is important to take into account that the drug can have an inhibitory effect on the contractile activity of the uterus.

In preclinical studies, it was found that fenoterol is excreted in mother's milk, but its effect on the development of an infant has not been studied. In this regard, during lactation, Berotek N is used only if the benefits are higher than the possible risks.

Clinical studies on the effects of fenoterol on fertility have not been conducted. In preclinical studies, no adverse effects of the drug on fertility have been identified.

Pediatric use

Berotek N is contraindicated in children under 4 years of age. Clinical experience with the use of the drug in children 4–12 years old is limited, therefore, at this age, treatment is carried out with caution, under close medical supervision and adult supervision.

Drug interactions

The side effects of fenoterol can be enhanced by glucocorticosteroids, anticholinergics, beta-adrenomimetics, diuretics, xanthine derivatives (eg, theophylline), cromoglycic acid.

Beta-blockers can significantly weaken the bronchodilator effect of fenoterol.

Tricyclic antidepressants and MAO inhibitors can enhance the effects of β-adrenergic receptor agonists, therefore, they should be used with caution during bronchodilator therapy.

Inhalation anesthetics (eg, enflurane, trichlorethylene, halothane) increase the risk of cardiovascular exposure to fenoterol.

Hypokalemia developed under the influence of Berotek N can be enhanced by corticosteroids, diuretics, xanthine derivatives. This phenomenon is of particular clinical importance in patients with severe airway obstruction.

Analogs

The analogues of Beroteka N are: Atimos, Astalin, Berotek, Ventolin, Vertasort, Clenbuterol, Kombipek, Onbrez Breezhaler, Oxis Turbuhaler, Salbutamol, Salgim, Foradil, Formoterol-native, Cybutol Cyclocaps and others.

Terms and conditions of storage

Keep out of reach of children, where temperature does not exceed 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Berotek N

Patients leave positive reviews about Berotek N, noting its effectiveness and rapid action in attacks of bronchial asthma and airway obstruction.

Price for Berotek N in pharmacies

The approximate price for Berotek N for 1 bottle of 10 ml (200 aerosol doses), depending on the place of sale, is 388-546 rubles.

Berotek N: prices in online pharmacies

Drug name Price Pharmacy

Berotek N 100 μg / dose 200 doses aerosol for inhalation metered dose 10 ml 1 pc. 374 r Buy

Berotek N aerosol for in. dosage. 100mcg / dose 200 doses 10ml 469 r Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!